Using radioligand binding assays, both α
1 and β adrenergic receptors of the human normal and hypertrophied prostatic tissue were quantitated, for the first time. For α
1 adrenergic receptor assay, with
3H-prazosin as a ligand, the prostatic crude membrane fraction were incubated for 20min. at 30°C with or without 10μM phentolamine. The number of binding sites (NBS) and the dissociation constant (Kd) were calculated from the Scatchard analysis.
The number of binding sites of α
1 adrenergic receptors in the normal prostatic tissue was determined 35.7±12.7fmol/mg protein (mean±S. D.), on the other hand, the NBS of it in the hypertrophied prostatic tissue was 50.3±14.6fmol/mg protein. In the hypertrophied prostate it was noticed that there was a significantly greater density of α
1 adrenergic receptors than in normal prostate (p<0.05), although there was no difference in Kd between them.
It has recently been revealed that the human prostatic smooth muscle elicited supersensitive contractions to α
1 adrenergic stimulants in benign prostatic hypertrophy, in vivo and in vitro. This supersensitive reaction seems to be due to the increase of α
1 adrenergic receptors density in the hypertrophied prostatic tissue. Furthermore, it was speculated that the greater density of α
1 adrenergic receptors in the hypertrophied prostate was caused by the denervation effect in the tissue.
For β adrenergic receptor assay,
3H-DHA (dihydroalprenolol) was used as a ligand. Although the incubation was performed for 30min. at 25°C, the method of binding assay was similar to the α
1 adrenergic receptor assay. No difference in the NBS of β adrenergic receptors was revealed between normal and hypertrophied prostatic tissue. Lower affinity of β adrenergic receptors was obtained in the benign prostatic hypertrophy than normal prostate.
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